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BENZOIMIDAZOLES AS PROLYL HYDROXYLASE INHIBITORS
专利权人:
JANSSEN FARMATSEVTIKA NV
发明人:
KhOUKATT Frehnsis Meredit (US),ХОУКАТТ Фрэнсис Мередит (US),LEONARD Barri Istman (US),ЛЕОНАРД Барри Истман (US),PEL'T'ER Khillari M. (US),ПЕЛЬТЬЕР Хиллари М. (US),FUONG Viktor K. (US),ФУОНГ Виктор К.,KHOUKATT FREHNSIS MEREDIT,ХОУКАТТ Фрэнсис Мередит,LEONARD BARRI ISTMAN,ЛЕОНАРД Барри Истман,PELTER KHILLARI M.,ПЕЛЬТЬЕР Хиллари М.,FUONG VIKTOR K.,RABINOVICH MAJKL KH.,РАБИНОВИЧ Майкл
申请号:
RU2010148421/04
公开号:
RU0002531354C2
申请日:
2009.04.28
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to the field of organic chemistry, namely to benzoimidazole derivatives of formula (I), as well as to their enantiomers, diastereoisomers, racemates and pharmaceutically acceptable salts, where n equals from 2 to 4, each of R1 substituents is independently selected from H, halogen, -C1-4alkyl, -C1-4pergaloalkyl, trifluoro-C1-4alkoxy, -NO2, -CN, CO2H, -OC1-4alkyl, -SC1-4alkyl, -S(C1-4alkyl)-Rc, -S(O)2(C1-4alkyl)-Rc, -S(O)-C1-4alkyl, -SO2-C1-4alkyl, -S-Rc, -S(O)-Rc, -SO2-Rc, -SO2-NH-Rc, -O-Rc, -CH2-O-Rc, -C(O)NH-Rc, -NRaRb, benzyloxy, phenyl, optionally substituted with one-two Rd, cyanobiphenyl-4-ylmethylsulpfanyl, cyanobiphenyl-4-ylmethanesulphonyl, or -S-(CH2)2-morpholine and two adjacent groups R1 can bind with formation of an aromatic 5-6-membered ring, optionally substituted with one methyl group or two atoms of halogen, optionally containing one or two S or N; Ra and Rb each independently represents C1-4alkyl, -C(O)C1-4alkyl, -C(O)-Rc, -C(O)CH2-Re, C1-4alkyl-Re, -SO2-Rc, -SO2-C1-4alkyl, phenyl, benzyl; or Ra and Rb together with a nitrogen atom, which they are bound with, form a monocyclic 5-6- membered heterocycloalkyl ring, optionally containing one heteroatom, selected from O; Rc represents -C3-8cycloalkyl, phenyl, optionally substituted with one-two Rd, benzyl, optionally substituted with one-three Rd; morpholine; Rd independently represents halogen, -OH, -C1-4alkyl or -C1-4perhalogenalkyl, trifluorine C1-4alcoxy, -OC1-4alkyl, or -O-benzyl optionally substituted with halogen, Re represents -C6heterocycloalkyl, optionally containing one or two of O or N atoms, optionally substituted with a methyl group; R2 and R3 both represent H, -CF3 or C1-3alkyl; each of Z represents a C or N atom, on condition that simultaneously not more than two Z represent N. The invention also relates to particular compounds, a pharmaceutical composition, based on formula (I) compound or a particular said compound, a method of treating d
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